Clotrimazole - 10mM in DMSO, high purity , CAS No.23593-75-1(DMSO)

2 Citations
Item Number
C408420
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C408420-1ml
1ml
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$47.90

Fungal Inhibitors

Basic Description

Specifications & Purity10mM in DMSO
Storage TempStore at -80°C
Shipped InIce chest + Ice pads
GradeMoligand™
Product Description

Information

Clotrimazole Clotrimazole (BAY b 5097, FB 5097) alters the permeability of the fungal cell wall by inhibiting the biosynthesis of ergosterol, used in the treatment of fungal infections.
In vitro

Clotrimazole causes a sustained depletion of intracellular Ca2+ stores, which results in activation of PKR, phosphorylation of eIF2alpha, and thereby in inhibition of protein synthesis at the level of translation initiation. Clotrimazole preferentially decreases the expression of the growth promoting proteins cyclin A, E and D1, resulting in inhibition of cyclin-dependent kinase activity and blockage of cell cycle in G1. Clotrimazole inhibits ADP-ribose-activated currents in HEK-293 cells expressing recombinant human TRPM2(hTRPM2). Clotrimazole (3 mM to 30 mM) produces an essentially complete inhibition of theTRPM2-mediated current. Clotrimazole antagonizes ADP-ribose-activated whole-cell and single-channel currents in the rat insulinoma cell-line CRI-G1. Clotrimazole (2 mM) causes a sharp decline in parasitemia, complete inhibition of parasite replication, and destruction of parasites and host cells within a single intraerythrocytic asexual cycle (approximately 48 hours). Clotrimazole effectively and rapidly inhibits parasite growth in five different strains of P. falciparum, in vitro, irrespective of their Chloroquine sensitivity.

In vivo

Clotrimazole stimulates a subset of capsaicin-sensitive and mustard oil-sensitive trigeminal neurons, and evoked nocifensive behavior and thermal hypersensitivity with intraplantar injection in mice. Clotrimazole-induced pain behavior is suppressed by the TRPV1-antagonist BCTC [(N-(-4-tertiarybutylphenyl)-4-(3-cholorpyridin-2-yl)tetrahydropyrazine-1(2H)-carboxamide)] and absent in TRPV1-deficient mice. Clotrimazole inhibits the cold and menthol receptor TRPM8, and blocks menthol-induced responses in capsaicin- and mustard oil-insensitive trigeminal neurons.
Cell Data

cell lines:

Concentrations:

Incubation Time:

Powder Purity:≥99%

Associated Targets(Human)

CYP2D6 Tclin Cytochrome P450 2D6 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CYP2C8 Tchem Cytochrome P450 2C8 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CYP8B1 Tchem 7-alpha-hydroxycholest-4-en-3-one 12-alpha-hydroxylase (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CYP2C19 Tchem Cytochrome P450 2C19 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CYP3A4 Tclin Cytochrome P450 3A4 (8 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CYP51A1 Tchem Lanosterol 14-alpha demethylase (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CYP2C9 Tchem Cytochrome P450 2C9 (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
TRPM2 Tchem Transient receptor potential cation channel subfamily M member 2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
TBXAS1 Tchem Thromboxane-A synthase (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
NR1I3 Tchem Nuclear receptor subfamily 1 group I member 3 (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CACNA1C Tclin Voltage-dependent L-type calcium channel subunit alpha-1C (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CYP19A1 Tclin Aromatase (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CYP17A1 Tclin Steroid 17-alpha-hydroxylase/17,20 lyase (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
KCNN4 Tchem Intermediate conductance calcium-activated potassium channel protein 4 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
KCNA3 Tclin Potassium voltage-gated channel subfamily A member 3 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

Canonical SMILES ClC1=C(C=CC=C1)C([N]2C=CN=C2)(C3=CC=CC=C3)C4=CC=CC=C4
Molecular Weight 344.84

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 100 mg/mL (155.58 mM);    

Related Documents

Citations of This Product

1. Guowei Li, Kai Lv, Xiangjun Pan, Siting Zhou, Hui Xing, Jun Xu, Dong Ma, Yunfeng Hu, Hao Xu.  (2023)  Dynamic nitric oxide/drug codelivery system based on polyrotaxane architecture for effective treatment of Candida albicans infection.  Acta Biomaterialia,  155  (618).  [PMID:36371005]
2. Xiaolei Wang, Hong Lu, Qiansheng Li, Yang Zhou, Jiti Zhou.  (2022)  Comparative genome and transcriptome of Rhodococcus pyridinivorans GF3 for analyzing the detoxification mechanism of anthraquinone compounds.  ECOTOXICOLOGY AND ENVIRONMENTAL SAFETY,  237  (113545).  [PMID:35453018]

References

1. Guowei Li, Kai Lv, Xiangjun Pan, Siting Zhou, Hui Xing, Jun Xu, Dong Ma, Yunfeng Hu, Hao Xu.  (2023)  Dynamic nitric oxide/drug codelivery system based on polyrotaxane architecture for effective treatment of Candida albicans infection.  Acta Biomaterialia,  155  (618).  [PMID:36371005]
2. Xiaolei Wang, Hong Lu, Qiansheng Li, Yang Zhou, Jiti Zhou.  (2022)  Comparative genome and transcriptome of Rhodococcus pyridinivorans GF3 for analyzing the detoxification mechanism of anthraquinone compounds.  ECOTOXICOLOGY AND ENVIRONMENTAL SAFETY,  237  (113545).  [PMID:35453018]

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